2. Apoptosis Metabolic Enzyme/Protease
  3. Apoptosis Carbonic Anhydrase NEDD8-activating Enzyme
  4. TAS4464

TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.).

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TAS4464

TAS4464 構造式

CAS 番号 : 1848959-10-3

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 201 在庫あり
Solution
10 mM * 1 mL in DMSO USD 201 在庫あり
Solid
5 mg $180 在庫あり
10 mg $290 在庫あり
25 mg $580 在庫あり
50 mg   お問い合わせ  
100 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 9 publication(s) in Google Scholar

Other Forms of TAS4464:

TAS4464 関連抗体

Top Publications Citing Use of Products

Carbonic Anhydrase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
CA CA I CA Ⅱ CA IX CA XII CA VII CA VI CA VA CA VB CA XIII CA XIV

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.)[1].

IC50 & Target

IC50：0.955 nM (NAE)[1]
体外実験

TAS4464 is a highly potent and selective recombinant NAE inhibitor, with over 470-fold and 1340-fold selectivity against recombinant UAE and SAE, respectively, and weak off-target inhibitory activity against CA2[1].
TAS4464 (1-10 μM; 24-48 h) induces apoptosis in leukemia, lymphoma, multiple myeloma and solid tumor cell lines, with the apoptosis rate increasing as the drug concentration rises[1].
TAS4464 (1 nM-1 μM, 4 h; 100 nM, 1-24 h) significantly increases the protein expression levels of CRL ubiquitin ligase substrates CDT1, p27, and phosphorylated IκBα in tumor cells, while reduces the level of cullin neddylation modification[1].
TAS4464 (0.1-10 μM; 24-48 h) significantly inhibits the migratory capacity of solid tumor cell lines such as colorectal cancer and sarcoma, with a concentration-dependent inhibitory effect[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TAS4464 関連抗体
体内実験

TAS4464 (25-100 mg/kg; i.v.; twice weekly; 3 weeks) hydrochloride achieves complete tumor regression and induces apoptosis in models of T-cell acute lymphoblastic leukemia (25 mg/kg), mantle cell lymphoma (100 mg/kg), clear cell sarcoma (100 mg/kg), and small cell lung cancer (75 mg/kg), with a broad selective window[1].
TAS4464 (100 mg/kg; i.v.; administered on days 1, 4, 8 and 11, with one cycle every 21 days; 8 cycles total) hydrochloride significantly prolongs survival and reduces tumor burden in a systemic diffuse large B-cell lymphoma model of SCID mice xenografted with TMD8-Luc[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

506.51

分子式

C21H23FN6O6S
CAS 番号
Appearance

Solid

Color

Off-white to light yellow

SMILES

NC1=NC=NC2=C1C(C#CC3=C(F)C=CC=C3OCC)=CN2[C@@H]4O[C@H](CNS(=O)(N)=O)[C@@H](O)[C@H]4O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 40 mg/mL (78.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9743 mL 9.8715 mL 19.7429 mL
5 mM 0.3949 mL 1.9743 mL 3.9486 mL
10 mM 0.1974 mL 0.9871 mL 1.9743 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2 mg/mL (3.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2 mg/mL (3.95 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.21%

COA (260 KB) HNMR (148 KB) LCMS (94 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9743 mL 9.8715 mL 19.7429 mL 49.3574 mL
5 mM 0.3949 mL 1.9743 mL 3.9486 mL 9.8715 mL
10 mM 0.1974 mL 0.9871 mL 1.9743 mL 4.9357 mL
15 mM 0.1316 mL 0.6581 mL 1.3162 mL 3.2905 mL
20 mM 0.0987 mL 0.4936 mL 0.9871 mL 2.4679 mL
25 mM 0.0790 mL 0.3949 mL 0.7897 mL 1.9743 mL
30 mM 0.0658 mL 0.3290 mL 0.6581 mL 1.6452 mL
40 mM 0.0494 mL 0.2468 mL 0.4936 mL 1.2339 mL
50 mM 0.0395 mL 0.1974 mL 0.3949 mL 0.9871 mL
60 mM 0.0329 mL 0.1645 mL 0.3290 mL 0.8226 mL
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TAS4464 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TAS44641848959-10-3TAS 4464TAS-4464ApoptosisCarbonic AnhydraseNEDD8-activating EnzymeCarbonate dehydrataseNAEInhibitorinhibitorinhibit

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TAS4464
製品番号:
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